Imiquimod (imiquimod) for non nucleoside heterocyclic amines new, chemical name 1- (2- methyl propyl) -4- amino -1 H- [4,5-C] quinoline and
Imiquimod (imiquimod) for non nucleoside heterocyclic amines new, chemical name 1- (2- methyl propyl) -4- amino -1 H- [4,5-C] quinoline and imiquimod. 5% Imiquimod Cream is the first topical immune in 1997 was approved by FDA in the treatment of external genital warts regulating drugs produced by the United States 3M pharmaceutical limited company, the name Aldara. Domestic Imiquimod Cream brand name Ming Xin Di cream. As a new type of topical immunomodulator imiquimod in treatment of condyloma acuminatum with good effect, safe use, low recurrence rate. Imiquimod and anti herpes virus and the treatment of some skin tumors, and indications are expanding. For the treatment of infantile hemangioma, also achieved a certain effect. Imiquimod cream (cream) only 5% preparations per gram of ointment containing imiquimod 50mg.
Imiquimod in the treatment of infantile hemangioma, first by Martinez MI is equal to 2002 seventh "dermatology Yearbook" on the report of Martinez MI, Sanchez-Carpintero I, North PE, Mihm MC Jr. Clinica Las Americas, San Juan de Puerto Rico. Infantile hemangioma: clinical resolution with 5% imiquimod cream. Arch Dermatol. 2002 Jul; 138 (7 884): 881-4; discussion; subsequently, American scholar Hazen in "pediatric dermatology" magazine published papers, Hazen PG, Carney JF, Engstrom CW, Turgeon KL, Reep MD, Tanphaichitr A. Department of Dermatology, Case-Western Reserve University School of Medicine, Cleveland, Ohio, USA.Paulhazen@aol.com. Proliferating hemangioma of infancy: successful treatment with topical imiquimod cream. Pediatr Dermatol. 2005 May- 5% Jun; 22 (3): 254-6.]. In July this year, held in Milan in the sixteenth session of the ISSVA conference, Spain and Canada doctors were reported efficacy of imiquimod in the treatment of infant hemangioma and precautions. From the current report on the clinical application of small, have certain curative effect of imiquimod in treatment of infantile hemangioma (Topical imiquimod cream appears to be a safe and effective therapy for rapidly enlarging proliferating hemangioma), especially suitable for medium and small body hidden parts of the treatment of hemangioma. The main advantage is that the drug is convenient, controllable, no local irritation, no systemic adverse reactions. The medication method is every other day for 3 ~ 1 times when, after 5 months of hemangiomas disappear completely, well tolerated.
1 pharmacological action
Imiquimod can enhance cellular immune activity in local drug induced inflammation and cytokines produced by immune regulation play indirect antiviral effect. Imiquimod can effectively induce in vivo including interferon alpha (IFN alpha) and tumor necrosis factor alpha (TNF alpha), cytokines. In vitro experiments, imiquimod can induce human peripheral mononuclear cells to produce IFN alpha, alpha TNF, alpha IL - 1, IL - 1, -6, IL beta 8, IL - 10, GM - CSF, MCP - 1 alpha (monocyte chemoattractant protein -1 alpha, MCP) - 1 beta cells.
Imiquimod Cream topical (0.05 g/ cm2) after 1h, the concentration of local skin IFN alpha and TNF alpha peak. Imiquimod 2 metabolites of S -26704 and S -22770, have similar immune activity. HPV can enter the body through the skin surface scratches tiny, after a period of latency (usually 3 to 8 weeks) after the formation of the wart, a small amount of imiquimod can penetrate the skin surface, induced by interferon. Through this activity of interferon antiviral factor HPV virus proliferation, inhibition of HPV infected keratinocytes proliferation. Imiquimod induced cytokine induced the nuclear and other white blood cells to the wart tissue chemotaxis to HPV antigen processing and activation of dendritic cells, presenting to the lymph nodes, the activation of HPV specific T lymphocytes in the lymph node is released into the blood. HPV specific T lymphocytes into the wart body, kill HPV infected cells, monocytes and macrophages to further engulf the debris. Through the establishment of HPV specific T lymphocyte immune memory, rapid treatment of any type of HPV infection, and then significantly reduce the recurrence rate of condyloma acuminatum.
2 in vitro and in vivo
Imiquimod Cream's largest concentration of 18.3%, according to the 110g/kg administration of rabbits were topical toxicity test, administered continuously for 1 weeks, except for slight erythema, no skin irritation, no sensitization effect on the skin of guinea pigs. In addition, animal experiments proved that imiquimod non carcinogenic, mutagenic, teratogenic effect. Show skin tolerance test, imiquimod no irritation to normal skin. With radiolabeled technology in 7 cases with imiquimod patients, found that the absorption is few, after application in serum was not detected in drugs, only in the urine and feces was measured 2%.
6 healthy subjects received a single topical 5mg 14C labeled Imiquimod Cream, research shows that 14C labeled imiquimod percutaneous absorption and rarely. Topical application of imiquimod, did not detect radioactive material in serum (detection limit: 1 g/mL), 0.9% radioactive material in urine and feces is less than the amount of radiolabeled.
4 adverse reactions
5% imiquimod cream and no adverse reaction was found in the system in the treatment of systemic adverse reactions without interferon fever, flu like symptoms, will not damage the skin tissue. However, in the mucosa, semi mucosa, soft tissue, so there are some light, moderate stimulation. The most common is erythema, accounting for about 61%, erosion accounted for about 30%, peeling accounted for about 23%, edema accounted for about 14%. Local stimulation of inflammation often occurs in second ~ 5 weeks, mostly light, moderate, short duration, about 4 ~ 12D, the general withdrawal of the drug after the stimulus response of 7 ~ 12D disappear. Can also have some subjective symptoms, such as itching, burning about 22%, accounting for about 13%, accounting for about 5% of the pain and tenderness.